GW 4064

Cat. No. 2473

GW 4064 C28H22Cl3NO4 [278779-30-9]

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Chemical Name: 3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid

Biological Activity

Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 μM. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

Soluble to 100 mM in DMSO and to 10 mM in ethanol
>97 %
Desiccate at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Lee et al (2014) Nutrient-sensing nuclear receptors coordinate autophagy. Nature 516 112. PMID: 25383539.

Cariou et al (2006) The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice. J.Biol.Chem. 281 11039. PMID: 16446356.

Zhang et al (2006) Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc.Natl.Acad.Sci.USA 103 1006.

Maloney et al (2000) Identification of a chemical tool for the orphan nuclear receptor FXR. J.Med.Chem. 43 2971. PMID: 10956205.

If you know of a relevant reference for GW 4064 please let us know.

Citations are publications that use Tocris products. Selected citations for GW 4064 include:

Gomez-Ospina et al (2016) Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis. J Hematol Oncol 7 10713. PMID: 26888176.

Kim et al (2016) The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation Scientific Reports 6 37280. PMID: 27869139.

Hoeke et al (2014) Human FXR regulates SHP expression through direct binding to an LRH-1 binding site, independent of an IR-1 and LRH-1. PLoS One 9 e88011. PMID: 24498423.

Lee et al (2014) Nutrient-sensing nuclear receptors coordinate autophagy. Nature 516 112. PMID: 25383539.

Rondini et al (2014) Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells. J Clin Invest 42 361. PMID: 24335393.

Dai et al (2011) Impact of bile acids on the growth of human cholangiocarcinoma via FXR. Drug Metab Dispos 4 41. PMID: 21988803.

Fu et al (2011) Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway. Proc Natl Acad Sci U S A 108 1403. PMID: 21220320.

Fickert et al (2009) Farnesoid X receptor critically determines the fibrotic response in mice but is expressed to a low extent in human hepatic stellate cells and periductal myofibroblasts. Am J Pathol 175 2392. PMID: 19910507.

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Keywords: GW 4064, supplier, Selective, farnesoid, X, receptor, FXR, agonists, Receptors, Liver, LXR-like, GW4064, GlaxoSmithKline, GSK, Tocris Bioscience, LXR-like Receptor Agonist products

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